AU2011281546B2 - 2,3,5-trisubstituted thiophene compounds and uses thereof - Google Patents

2,3,5-trisubstituted thiophene compounds and uses thereof Download PDF

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Publication number
AU2011281546B2
AU2011281546B2 AU2011281546A AU2011281546A AU2011281546B2 AU 2011281546 B2 AU2011281546 B2 AU 2011281546B2 AU 2011281546 A AU2011281546 A AU 2011281546A AU 2011281546 A AU2011281546 A AU 2011281546A AU 2011281546 B2 AU2011281546 B2 AU 2011281546B2
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Prior art keywords
cyclohexyl
oxo
thiophene
carboxylic acid
dimethyl
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Expired - Fee Related
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AU2011281546A
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AU2011281546A1 (en
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David Barnes
Scott Louis Cohen
Jiping Fu
Lei Shu
Rui Zheng
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Novartis AG
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Novartis AG
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A61K31/541Non-condensed thiazines containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/38Heterocyclic compounds having sulfur as a ring hetero atom
    • A61K31/381Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
    • AHUMAN NECESSITIES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/4025Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/422Oxazoles not condensed and containing further heterocyclic rings
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4535Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
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    • C07D498/04Ortho-condensed systems

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  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
AU2011281546A 2010-07-22 2011-07-21 2,3,5-trisubstituted thiophene compounds and uses thereof Expired - Fee Related AU2011281546B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US36668710P 2010-07-22 2010-07-22
US61/366,687 2010-07-22
US42334610P 2010-12-15 2010-12-15
US61/423,346 2010-12-15
PCT/EP2011/062545 WO2012010663A1 (fr) 2010-07-22 2011-07-21 Composés de thiophène 2,3,5-trisubstitués et leurs utilisations

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AU2011281546A1 AU2011281546A1 (en) 2013-01-31
AU2011281546B2 true AU2011281546B2 (en) 2014-07-10

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US (2) US9040690B2 (fr)
EP (1) EP2595983A1 (fr)
JP (1) JP5650324B2 (fr)
KR (1) KR20130131301A (fr)
CN (1) CN103025728B (fr)
AU (1) AU2011281546B2 (fr)
BR (1) BR112013001516A2 (fr)
CA (1) CA2806108A1 (fr)
CL (1) CL2013000210A1 (fr)
CO (1) CO6680616A2 (fr)
CR (1) CR20130029A (fr)
EA (1) EA201300160A1 (fr)
GT (1) GT201300024A (fr)
MA (1) MA34462B1 (fr)
MX (1) MX2013000906A (fr)
SG (1) SG187561A1 (fr)
TN (1) TN2012000617A1 (fr)
UY (1) UY33857A (fr)
WO (1) WO2012010663A1 (fr)

Families Citing this family (1)

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Publication number Priority date Publication date Assignee Title
CN107686475B (zh) * 2017-09-14 2020-09-25 湘潭大学 2,3,5-三取代噻吩及其衍生物的合成方法

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WO2008058393A1 (fr) * 2006-11-15 2008-05-22 Virochem Pharma Inc. Analogues du thiophène pour le traitement ou la prévention d'infections par un flavivirus
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WO2011068715A1 (fr) * 2009-11-25 2011-06-09 Vertex Pharmaceuticals Incorporated Dérivés d'acide 5-alcynyl-thiophène-2-carboxylique et leur utilisation pour traiter ou prévenir des infections à flavivirus

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WO2008058393A1 (fr) * 2006-11-15 2008-05-22 Virochem Pharma Inc. Analogues du thiophène pour le traitement ou la prévention d'infections par un flavivirus
GB2450771A (en) * 2007-04-12 2009-01-07 Angeletti P Ist Richerche Bio Heterocyclic compounds and their use as inhibitors of HCV polymersases for the treatment of HCV
US20110020278A1 (en) * 2009-07-21 2011-01-27 Gilead Sciences, Inc. Inhibitors of flaviviridae viruses
WO2011031669A1 (fr) * 2009-09-09 2011-03-17 Gilead Sciences, Inc. Inhibiteurs de virus de la famille des flaviviridae
WO2011068715A1 (fr) * 2009-11-25 2011-06-09 Vertex Pharmaceuticals Incorporated Dérivés d'acide 5-alcynyl-thiophène-2-carboxylique et leur utilisation pour traiter ou prévenir des infections à flavivirus

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US20130123252A1 (en) 2013-05-16
MA34462B1 (fr) 2013-08-01
MX2013000906A (es) 2013-02-27
CA2806108A1 (fr) 2012-01-26
WO2012010663A1 (fr) 2012-01-26
JP2013535442A (ja) 2013-09-12
AU2011281546A1 (en) 2013-01-31
KR20130131301A (ko) 2013-12-03
SG187561A1 (en) 2013-03-28
CN103025728B (zh) 2015-11-25
US9498483B2 (en) 2016-11-22
CN103025728A (zh) 2013-04-03
CR20130029A (es) 2013-04-17
WO2012010663A9 (fr) 2013-01-24
CL2013000210A1 (es) 2013-05-03
US20150224109A1 (en) 2015-08-13
CO6680616A2 (es) 2013-05-31
BR112013001516A2 (pt) 2016-06-07
GT201300024A (es) 2016-06-07
EP2595983A1 (fr) 2013-05-29
EA201300160A1 (ru) 2013-06-28
JP5650324B2 (ja) 2015-01-07
UY33857A (es) 2013-02-28
TN2012000617A1 (en) 2014-04-01
US9040690B2 (en) 2015-05-26

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